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公开(公告)号:US6153590A
公开(公告)日:2000-11-28
申请号:US930584
申请日:1998-02-02
申请人: Raymond Andersen , John Coleman , Dilip De Silva , Fangming Kong , Edward Piers , Debra Wallace , Michel Roberge , Teresa Allen
发明人: Raymond Andersen , John Coleman , Dilip De Silva , Fangming Kong , Edward Piers , Debra Wallace , Michel Roberge , Teresa Allen
CPC分类号: C07K5/0205 , C07K5/0827 , A61K38/00
摘要: Compounds of general formula I ##STR1## wherein: R.sub.1 and R.sub.70 independently represent a hydrogen atom or an optionally substituted alkyl or acyl group; R.sub.2 represents a hydrogen atom or an optionally substituted alkyl or acyl group or is absent when R.sub.6 represents a group --CH.dbd. as hereinafter described; R.sub.73 represents a hydrogen atom or an optional substituent or is absent when R.sub.6 represents a methylene group or a group --CH.dbd. as hereinafter described; Y represents an optional substituent; n represents 0, 1, 2, 3, or 4; R.sub.3 represents a hydrogen atom, or an optionally substituted alkyl group; R.sub.74 represents a hydrogen atom, a hydroxy group or an optionally substituted alkyl or acyl group; R.sub.7 represents a hydrogen atom or an alkyl group; R.sub.75 represents an optionally substituted alkyl group; and i) R.sub.6 and R.sub.71 independently represent a hydrogen atom or an optionally substituted alkyl or acyl group; and R.sub.72 represents a hydrogen atom; or ii) R.sub.71 represents a hydrogen atom or an optionally susbtituted alkyl or acyl group and R.sub.72 represents a hydrogen atom or R.sub.71 and R.sub.72 are joined together such that a double bond is formed between the carbon atoms to which they are attached; and R.sub.6 represents an optionally substituted methylene group bonded to the indole moiety thereby forming a tricyclic moiety; or R.sub.6 represents an optionally substituted group --CH.dbd. bonded to the indole moiety thereby to form an aromatic tricyclic moiety; for use in therapy and as antimitotic reagents are described.
摘要翻译: PCT No.PCT / GB96 / 00942 Sec。 371日期1998年2月2日 102(e)1998年2月2日PCT 1996年4月22日PCT PCT。 出版物WO96 / 33211 日期:1996年10月24日通式I化合物其中:R 1和R 70独立地表示氢原子或任选取代的烷基或酰基; R2表示氢原子或任选取代的烷基或酰基,或当R6表示基团-CH =时不存在,如下所述; 当R 6表示亚甲基或-CH =如下所述时,R 73表示氢原子或任选的取代基或不存在; Y表示任选的取代基; n表示0,1,2,3或4; R3表示氢原子或任选取代的烷基; R 74表示氢原子,羟基或任选取代的烷基或酰基; R7表示氢原子或烷基; R75表示任选取代的烷基; 和i)R 6和R 71独立地表示氢原子或任选取代的烷基或酰基; R 72表示氢原子; 或ii)R 71表示氢原子或任选取代的烷基或酰基,R 72表示氢原子或R 71和R 72连接在一起,使得在它们所连接的碳原子之间形成双键; 并且R 6表示与吲哚部分键合的任选取代的亚甲基,从而形成三环部分; 或R6表示与吲哚部分键合的任选取代的基团-CH =,从而形成芳族三环部分; 用于治疗和用作抗有益剂的试剂。
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公开(公告)号:US07410951B2
公开(公告)日:2008-08-12
申请号:US11034922
申请日:2005-01-14
申请人: Raymond Andersen , John Coleman , Dilip De Silva , Fangming Kong , Edward Piers , Debra Wallace , Michel Roberge , Theresa Allen
发明人: Raymond Andersen , John Coleman , Dilip De Silva , Fangming Kong , Edward Piers , Debra Wallace , Michel Roberge , Theresa Allen
IPC分类号: C07K5/06
CPC分类号: C07K5/0205 , A61K38/00 , C07K5/0827
摘要: Derivatives of hemiasterlin or Geodiamolide G having anti-mitotic activities and useful in treating cancer. These derivatives are represented by formula I wherein Y, n, R1, R2, R3, R7, R70, R71, R72, R74, and R75 are as defined in the specification.
摘要翻译: 具有抗有丝分裂活性并可用于治疗癌症的半精球蛋白或地高二聚G的衍生物。 这些衍生物由式I表示,其中Y,n,R 1,R 2,R 3,R 7, ,R 70,R 71,R 72,R 74和R 75, SUB>如说明书中所定义。
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公开(公告)号:US07772397B2
公开(公告)日:2010-08-10
申请号:US12176716
申请日:2008-07-21
申请人: Raymond Andersen , John Coleman , Dilip De Silva , Fangming Kong , Edward Piers , Debra Wallace , Michel Roberge , Theresa Allen
发明人: Raymond Andersen , John Coleman , Dilip De Silva , Fangming Kong , Edward Piers , Debra Wallace , Michel Roberge , Theresa Allen
IPC分类号: C07D471/04
CPC分类号: C07K5/0205 , A61K38/00 , C07K5/0827
摘要: This invention relates to derivatives of hemiasterlin or Geodiamolide G having anti-mitotic activities and useful in treating cancer. These derivatives are represented by general formula I, wherein Y, n, R1, R2, R3, R6, R7, R70, R71, R72, R74, and R75 are as defined in the specification.
摘要翻译: 本发明涉及具有抗有丝分裂活性并可用于治疗癌症的半球蛋白或衍生物的衍生物。 这些衍生物由通式I表示,其中Y,n,R 1,R 2,R 3,R 6,R 7,R 70,R 71,R 72,R 74和R 75如说明书中所定义。
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公开(公告)号:US20090088573A1
公开(公告)日:2009-04-02
申请号:US12176716
申请日:2008-07-21
申请人: Raymond ANDERSEN , John Coleman , Dilip De Silva , Fangming Kong , Edward Piers , Debra Wallace , Michel Roberge , Theresa Allen
发明人: Raymond ANDERSEN , John Coleman , Dilip De Silva , Fangming Kong , Edward Piers , Debra Wallace , Michel Roberge , Theresa Allen
IPC分类号: C07D471/04
CPC分类号: C07K5/0205 , A61K38/00 , C07K5/0827
摘要: This invention relates to derivatives of hemiasterlin or Geodiamolide G having anti-mitotic activities and useful in treating cancer. These derivatives are represented by general formula I, wherein Y, n, R1, R2, R3, R6, R7, R70, R71, R72, R74, and R75 are as defined in the specification.
摘要翻译: 本发明涉及具有抗有丝分裂活性并可用于治疗癌症的半球蛋白或衍生物的衍生物。 这些衍生物由通式I表示,其中Y,n,R 1,R 2,R 3,R 6,R 7,R 70,R 71,R 72,R 74和R 75如说明书中所定义。
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公开(公告)号:US20050171137A1
公开(公告)日:2005-08-04
申请号:US11034922
申请日:2005-01-14
申请人: Raymond Andersen , John Coleman , Dilip De Silva , Fangming Kong , Edward Piers , Debra Wallace , Michael Roberge , Teresa Allen
发明人: Raymond Andersen , John Coleman , Dilip De Silva , Fangming Kong , Edward Piers , Debra Wallace , Michael Roberge , Teresa Allen
IPC分类号: A61K38/00 , A61P35/00 , C07K5/02 , C07K5/027 , C07K5/078 , C07K5/08 , C07K5/083 , A61K31/4745 , C07D471/02
CPC分类号: C07K5/0205 , A61K38/00 , C07K5/0827
摘要: This invention relates to derivatives of hemiasterlin or Geodiamolide G having anti-mitotic activities and useful in treating cancer. These derivatives are represented by general formula I, wherein Y, n, R1, R2, R3, R6, R7, R70, R71, R72, R74, and R75 are as defined in the specification.
摘要翻译: 本发明涉及具有抗有丝分裂活性并可用于治疗癌症的半球蛋白或衍生物的衍生物。 这些衍生物由通式I表示,其中Y,n,R 1,R 2,R 3,R 6, R 7,R 70,R 71,R 72,R 74, / SUB>和R 75'如说明书中所定义。
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公开(公告)号:US06870028B1
公开(公告)日:2005-03-22
申请号:US09593417
申请日:2000-06-14
申请人: Raymond Andersen , John Coleman , Dilip De Silva , Fangming Kong , Edward Piers , Debra Wallace , Michael Roberge , Theresa Allen
发明人: Raymond Andersen , John Coleman , Dilip De Silva , Fangming Kong , Edward Piers , Debra Wallace , Michael Roberge , Theresa Allen
CPC分类号: C07K5/0205 , A61K38/00 , C07K5/0827
摘要: This invention relates to derivatives of hemiasterlin or Geodiamolide G having anti-mitotic activities and useful in treating cancer. These derivatives are represented by general formula I, wherein Y, n, R1, R2, R3, R6, R7, R70, R71, R72, R74, and R75 are as defined in the specification.
摘要翻译: 本发明涉及具有抗有丝分裂活性并可用于治疗癌症的半球蛋白或衍生物的衍生物。 这些衍生物由通式I表示,其中Y,n,R 1,R 2,R 3,R 6,R 7,R 70,R 71,R 72,R 74和R 75如说明书中所定义。
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